Expiration date: 04/2025

Form and composition:

Tablets white or almost white, round, flat, with beveled edges and embossed TS on one side and the dividing risk - on the other side of the tablet.

1 tablet contains:

atenolol 50 mg

amlodipine 5 mg

Excipients: isopropanol, calcium hydrogen phosphate (calcium phosphate dwuhosnovny), sodium starch of glycolate, corn starch, silica colloidal anhydrous, magnesium stearate, povidone-30, purified talc, cellulose microcrystalline.

10 PCs. - blisters (1) - cardboard packs.

10 PCs. - blisters (2) - cardboard packs.

10 PCs. - blisters (3) - cardboard packs.

14 PCs. - blisters (1) - cardboard packs.

14 PCs. - blisters (2) - cardboard packs.

14 PCs. - blisters (3) - cardboard packs

Pharmacological action:

Combined drug, the effect of which is due to the properties of its components.

Atenolol - a cardioselective beta1-blocker, exerts antianginal, antihypertensive and antiarrhythmic action. Has no membrane stabilizing and intrinsic sympathomimetic activity. Reduces the formation of camp and ATP stimulated by catecholamines, reduces intracellular current of calcium ions. In the first 24 hours after ingestion, against the background of a decrease in cardiac output, there is a reactive increase in OPSS, the severity of which gradually decreases within 1-3 days.

The antihypertensive effect is associated with a decrease in cardiac output, a decrease in the activity of the renin-angiotensin system, sensitivity of baroreceptors and the effect on the Central nervous system. Hypotensive effect is manifested by a decrease in systolic and diastolic blood PRESSURE, a decrease in shock and minute volume. When used in medium recommended doses has no effect on the tone of the peripheral arteries. Hypotensive effect persists 24 hours, with regular use of blood PRESSURE is stabilized by the end of 2 weeks of treatment.

The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening of diastole and improving myocardial perfusion) and a decrease in myocardial contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces heart rate at rest and during exercise. By increasing the tension of ventricular muscle fibers and end-diastolic pressure in the left ventricle may increase myocardial oxygen demand, especially in patients with chronic heart failure.

The negative chronotropic effect is manifested in 1 h after administration, reaches a maximum of 2-4 h and lasts up to 24 h.

Antiarrhythmic action is manifested by the suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic effects on the cardiac conduction system, inhibition of heterogeneous automatism, decrease in the speed of excitation propagation through the sinoatrial node and lengthening of the refractory period. It inhibits the conduction of pulses in the antegrade and to a lesser extent - retrograde directions through the AV node and along additional paths.

It increases the survival rate of patients with myocardial infarction (reduces the incidence of ventricular arrhythmias and angina attacks).

In therapeutic concentrations does not affect the beta2-adrenoceptors, unlike non-selective beta-blockers has a less pronounced effect on the smooth muscles of the bronchi, peripheral arteries and lipid metabolism. Slightly reduces the vital capacity of the lungs, practically does not weaken the bronchodilating effect of isoproterenol. When taking more than 100 mg/day may have an impact on beta2-adrenergic receptors.

Amlodipine - blocker of slow calcium channels, is a derivative of dihydropyridine. It has antihypertensive, antianginal, antispasmodic and vasodilator effect. Blocks the flow of calcium ions through cell membranes in smooth muscle cells of blood vessels and myocardium. The mechanism of antihypertensive action is due to the direct effect on the smooth muscles of the vessels.

The antianginal effect of amlodipine is due to the expanding effect on peripheral arterioles, which leads to a decrease in OPSS. At the same time, a decrease in the load on the heart leads to a decrease in myocardial oxygen demand, and simultaneously increases the flow of oxygen to the myocardium due to the expansion of the coronary arteries (which is especially important in angiospastic angina).

Amlodipine has no adverse effect on metabolism and lipid composition of blood plasma, has antiatherosclerotic, antithrombotic activity, increases the speed of glomerular filtration, has a weakly expressed natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria.

Pharmacokinetics:

Atenolol

Suction

After oral administration, atenolol is rapidly absorbed from the gastrointestinal tract (approximately 50% of the dose). Bioavailability-40-50%. Cmax is achieved through 2-4 h after oral administration.

Distribution

Poorly penetrates through the BBB and through the placental barrier, in small amounts is excreted in breast milk. The plasma protein binding is 6-16%.

Metabolism and excretion

Practically not biotransformed in the liver. Excreted by the kidneys by glomerular filtration, with 85-100% - unchanged. T1/2 is 6-9 hours.

Pharmacokinetics in special clinical cases

T1 / 2 in elderly patients increases. If impaired renal function the T1/2 increases and there is a cumulative effect. In patients with CC below 35 mg/min/1.73 m2 T1/2 is 16-27 h, when QC is below 15 mg/min/1.73 m2 more than 27 hours Displayed in hemodialysis.

Amlodipine

Suction

After taking the drug amlodipine inside quickly and almost completely (90%) absorbed from the gastrointestinal tract, Cmax achieved through 6-12 h. the Bioavailability of 60-65%.

Distribution

Css is set after 7-8 days of constant dose of the drug. Vd is 20 l / kg Binding to plasma proteins - more than 95%. Penetrates the GAB.

Metabolism and excretion

Biotransformed mainly in the liver to form inactive metabolites. Less than 10% is excreted unchanged, about 60% - in the form of inactive metabolites of the kidneys, 20-25% - in the form of metabolites with bile and through the intestine, as well as breast milk.

Indications:

• arterial hypertension
  
• prevention of angina attacks.
  

Dosage regimen:

With hypertension, the recommended dose is 1 tab./ day. If necessary, the daily dose can be increased to 2 tab./ day. The maximum daily dose - 2 tab.

You can not abruptly interrupt treatment because of the risk of severe arrhythmias and myocardial infarction, especially in patients with coronary artery disease. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (the dose is reduced by 25% in 3-4 days).

Tablets are taken orally, drinking the necessary amount of liquid.

Side effect:

On the part of the cardiovascular system: the appearance or worsening of symptoms of heart failure, violation of AV-conduction, bradycardia, marked decrease in blood PRESSURE, heartbeat, shortness of breath, blood flow to the skin, peripheral edema.

From the digestive system: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, hyperplasia of the gums rarely - increased activity of hepatic transaminases, cholestatic jaundice, dyspepsia.

From the Central and peripheral nervous system: dizziness, sleep disorders, decreased ability to concentrate, drowsiness, depression, hallucinations, lethargy, fatigue, headache rarely - mood changes, asthenia, visual impairment, paresthesia.

From the musculoskeletal system: muscle cramps, myalgia.

Respiratory system: dyspnea, bronchospasm, apnea.

From the hematopoietic system: thrombocytopenic purpura, anemia (aplastic), thrombosis.

From the endocrine system: decreased potency, decreased libido, gynecomastia, hyperlipidemia, hypoglycemia.

Dermatological reactions: urticaria, dermatitis, itching, photosensitivity, rarely - erythema multiforme exudative.

Other: increased urination.

The drug is usually well tolerated by patients.

Contraindications:

• severe arterial hypotension
  
• AV blockade II and III degree
  
• CVS
  
• sinoatrial blockade
  
• acute heart failure
  
• chronic heart failure stage II-III in the decompensation phase
  
• severe bradycardia
  
• metabolic acidosis
  
• bronchial asthma, chronic obstructive pulmonary disease
  
• prinzmetal
  
• cardiomegaly without signs of heart failure
  
• simultaneous reception of MAO inhibitors
  
• child and adolescence to 18 years
  
• hypersensitivity to the drug components.
  

Caution is prescribed for AV-blockade of the I degree, liver dysfunction, stenosis of the aorta mouth, chronic heart failure (in the compensation phase), chronic renal failure, pheochromocytoma, diabetes, hypoglycemia, thyrotoxicosis, obliterating peripheral vascular diseases (symptom of intermittent claudication, Raynaud's syndrome), myasthenia gravis, depression (including history), psoriasis, as well as elderly patients age.

Pregnancy and lactation:

During pregnancy Tanecek prescribed only in cases when the expected benefit to the mother outweighs the potential risk to the fetus.

During lactation (breastfeeding) the drug should be taken only in exceptional cases with great caution.

Special instruction:

In thyrotoxicosis, the drug can mask certain clinical signs of hyperthyroidism (for example, tachycardia). Tenochca abrupt withdrawal in patients with thyrotoxicosis is contraindicated, because it can reinforce the symptoms.

The drug slightly increases insulin-induced hypoglycemia and does not delay the restoration of glucose concentration in the blood to normal levels.

Selection of the drug dose in patients with chronic heart failure (compensated) should be carried out with caution.

If it is necessary to carry out surgery under General anesthesia, the drug should be discontinued for 48 hours before surgery. As an anesthetic, you should choose a drug with a possible minimum negative inotropic effect.

While the use of clonidine welcome Tenochca stop for a few days before clonidine to avoid withdrawal symptoms last.

It is possible to increase the severity of allergic reactions and the lack of effect of conventional doses of epinephrine in patients with a burdened allergic history.

Drugs that reduce the reserves of catecholamines (for example, reserpine), can enhance the action of beta-blockers, so patients receiving such a combination of drugs should be under constant supervision to identify a marked decrease in blood PRESSURE or bradycardia.

In the case of elderly patients with severe bradycardia (heart rate less than 50/min), a significant decrease in blood pressure (systolic blood PRESSURE below 100 mm Hg.Hg), AV blockade, bronchospasm, ventricular arrhythmias, severe violations of the liver and kidneys, it is necessary to reduce the dose or cancel Tanecek.

With the development of depression in the background of the drug is recommended to stop therapy.

If necessary, in/in the introduction verapamil is an introduction should be not less than 48 hours after the last ingestion Tenochca.

When using atenolol may reduce the production of lacrimal fluid, which is important for patients using contact lenses.

It should stop the drug before the study of concentration in blood and urine catecholamines, vanillylmandelic acid, titles of antinuclear antibodies.

In smokers, the effectiveness of beta-blockers is lower.

Control of laboratory parameters

It is necessary to control heart rate and blood pressure (at the beginning of treatment – daily, then 1 once in 3-4 mo), the concentration of blood glucose in patients with diabetes mellitus (1 once in 4-5 mo). In elderly people, it is recommended to evaluate renal function (1 time in 4-5 months).

It is necessary to teach the patient the technique of heart rate calculation and to instruct about the need for medical consultation at heart rate less than 50 UD. /min.

Impact on the ability to drive and operate machinery

Tanecek should be used with caution in patients, engaged in potentially hazardous activities, because of a possible reduction in concentration.

Overdose:

Symptoms: severe bradycardia, AV-blockade of II and III degree, increase in symptoms of heart failure, marked decrease in blood PRESSURE, bronchospasm, hypoglycemia.

Treatment: symptomatic. Hemodialysis is not effective.

Drug interaction:

While the use of insulin (or oral hypoglycemic agents) masked symptoms of hypoglycemia (due to the action of atenol).

In a joint application Tenochca with antihypertensive drugs of other groups is a mutual enhancement of the hypotensive effect.

Hypotensive effect of the drug weakens estrogens, GCS, mineralocorticoids, NSAIDs (due to sodium retention).

While the use of atenolol and cardiac glycosides increases the risk of bradycardia and violations of AV-conduction.

With the simultaneous appointment of atenolol with reserpine, methyldopa, clonidine, verapamil, it is possible to develop severe bradycardia.

When administered simultaneously with ergotamine and derivatives of xanthine efficacy of atenolol is reduced.

Concomitant use with lidocaine may slow the excretion of atenolol and amlodipine from the body and increase the risk of toxic effects of the drug.

Application in conjunction with phenothiazine derivatives increases the concentration of active substances in the blood serum.

Phenytoin (with/in the introduction) and funds for/in anesthesia increase the severity of cardiodepressive action of atenolol.

Allergens used for immunotherapy, or allergen extracts for skin samples and iodine-containing x-ray contrast agents for IV administration increase the risk of severe systemic allergic reactions or anaphylaxis.

Means for inhalation General anesthesia (derivatives of hydrocarbons) increase the risk of inhibition of myocardial function and a marked decrease in blood PRESSURE.

When used together, amiodarone increases the risk of bradycardia and slowing AV-conduction.

Cimetidine increases the concentration of atenolol in blood plasma (by inhibiting its metabolism).

In a joint application of Teocak nedepoliarizutmi to prolong the action of muscle relaxants and anticoagulant effect of coumarins.

Storage conditions and terms:

List B. the Drug should be stored in a dry, protected from light and out of reach of children at temperatures below 25°C.